Issue 11, 2014

Nucleolipids as building blocks for the synthesis of 99mTc-labeled nanoparticles functionalized with folic acid

Abstract

The development of drug delivery nanocarriers is emerging as a promising therapeutic tool to transport anti-cancer agents to tumors. In this contribution, preparation of nanoparticles (NPs) highly loaded with cisplatin using the bio-inspired hybrid nucleoside-lipids has been reported. The construction of these NPs using a “layer-by-layer’’ approach allows surface functionalization with polyethylene glycol and targeting moieties. Uridine moieties were pegylated for folic acid (FA) functionalisation to render specificity for active targeting. The uridine moieties at the surface of the nanoparticle act as ligands for 99mTc radiolabeling, whereas the lipid chains maintain the structure of the nanoparticle. In vitro, these hybrid NPs are stable and actively internalize in two different cell lines overexpressing the folic acid receptor. In vivo scintigraphy shows that nucleolipid functionalized NPs notably improved the pharmacokinetic profile of cisplatin (enhanced blood circulation time) and accumulated in the tumor xenografted mice model.

Graphical abstract: Nucleolipids as building blocks for the synthesis of 99mTc-labeled nanoparticles functionalized with folic acid

Supplementary files

Article information

Article type
Paper
Submitted
11 Apr 2014
Accepted
01 Aug 2014
First published
01 Aug 2014

New J. Chem., 2014,38, 5240-5246

Author version available

Nucleolipids as building blocks for the synthesis of 99mTc-labeled nanoparticles functionalized with folic acid

K. Oumzil, S. Khiati, M. Camplo, M. Koquely, K. Chuttani, S. Chaturvedi, A. K. Mishra and P. Barthélémy, New J. Chem., 2014, 38, 5240 DOI: 10.1039/C4NJ00559G

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